Publication

Screening multicomponent reactions for X-linked inhibitor of apoptosis-baculoviral inhibitor of apoptosis protein repeats domain binder

Monfardini, I., Huang, J-W., Beck, B., Cellitti, J. F., Pellecchia, M. & Dömling, A., 10-Feb-2011, In : Journal of Medicinal Chemistry. 54, 3, p. 890-900 11 p.

Research output: Contribution to journalArticleAcademicpeer-review

APA

Monfardini, I., Huang, J-W., Beck, B., Cellitti, J. F., Pellecchia, M., & Dömling, A. (2011). Screening multicomponent reactions for X-linked inhibitor of apoptosis-baculoviral inhibitor of apoptosis protein repeats domain binder. Journal of Medicinal Chemistry, 54(3), 890-900. https://doi.org/10.1021/jm101341m

Author

Monfardini, Ilaria ; Huang, Jui-Wen ; Beck, Barbara ; Cellitti, Jason F ; Pellecchia, Maurizio ; Dömling, Alexander. / Screening multicomponent reactions for X-linked inhibitor of apoptosis-baculoviral inhibitor of apoptosis protein repeats domain binder. In: Journal of Medicinal Chemistry. 2011 ; Vol. 54, No. 3. pp. 890-900.

Harvard

Monfardini, I, Huang, J-W, Beck, B, Cellitti, JF, Pellecchia, M & Dömling, A 2011, 'Screening multicomponent reactions for X-linked inhibitor of apoptosis-baculoviral inhibitor of apoptosis protein repeats domain binder', Journal of Medicinal Chemistry, vol. 54, no. 3, pp. 890-900. https://doi.org/10.1021/jm101341m

Standard

Screening multicomponent reactions for X-linked inhibitor of apoptosis-baculoviral inhibitor of apoptosis protein repeats domain binder. / Monfardini, Ilaria; Huang, Jui-Wen; Beck, Barbara; Cellitti, Jason F; Pellecchia, Maurizio; Dömling, Alexander.

In: Journal of Medicinal Chemistry, Vol. 54, No. 3, 10.02.2011, p. 890-900.

Research output: Contribution to journalArticleAcademicpeer-review

Vancouver

Monfardini I, Huang J-W, Beck B, Cellitti JF, Pellecchia M, Dömling A. Screening multicomponent reactions for X-linked inhibitor of apoptosis-baculoviral inhibitor of apoptosis protein repeats domain binder. Journal of Medicinal Chemistry. 2011 Feb 10;54(3):890-900. https://doi.org/10.1021/jm101341m


BibTeX

@article{8c79944049b8454c8c741a60dd5d9058,
title = "Screening multicomponent reactions for X-linked inhibitor of apoptosis-baculoviral inhibitor of apoptosis protein repeats domain binder",
abstract = "We report a second example of a general reaction screening approach to discover low molecular weight inhibitors of protein protein interactions. On the basis of the known pharmacophore model of SMAC mimetics, we predicted several inhibitors based on four different multicomponent reactions. The predicted inhibitors were subsequently synthesized, tested, and found to bind to the antiapoptotic protein X-linked inhibitor of apoptosis protein (XIAP) and showed cellular activity. Also the compounds are currently not highly potent. They could form a starting point for future medicinal chemistry optimization.",
keywords = "Amino Acid Motifs, Amino Acid Sequence, Antineoplastic Agents, Cell Line, Tumor, Cell Survival, Databases, Factual, Drug Screening Assays, Antitumor, Humans, Models, Molecular, Peptidomimetics, Piperazines, Protein Binding, Stereoisomerism, Structure-Activity Relationship, Tetrazoles, Thiazoles, Thiazolidines, X-Linked Inhibitor of Apoptosis Protein",
author = "Ilaria Monfardini and Jui-Wen Huang and Barbara Beck and Cellitti, {Jason F} and Maurizio Pellecchia and Alexander D{\"o}mling",
year = "2011",
month = feb,
day = "10",
doi = "10.1021/jm101341m",
language = "English",
volume = "54",
pages = "890--900",
journal = "Journal of Medicinal Chemistry",
issn = "0022-2623",
publisher = "AMER CHEMICAL SOC",
number = "3",

}

RIS

TY - JOUR

T1 - Screening multicomponent reactions for X-linked inhibitor of apoptosis-baculoviral inhibitor of apoptosis protein repeats domain binder

AU - Monfardini, Ilaria

AU - Huang, Jui-Wen

AU - Beck, Barbara

AU - Cellitti, Jason F

AU - Pellecchia, Maurizio

AU - Dömling, Alexander

PY - 2011/2/10

Y1 - 2011/2/10

N2 - We report a second example of a general reaction screening approach to discover low molecular weight inhibitors of protein protein interactions. On the basis of the known pharmacophore model of SMAC mimetics, we predicted several inhibitors based on four different multicomponent reactions. The predicted inhibitors were subsequently synthesized, tested, and found to bind to the antiapoptotic protein X-linked inhibitor of apoptosis protein (XIAP) and showed cellular activity. Also the compounds are currently not highly potent. They could form a starting point for future medicinal chemistry optimization.

AB - We report a second example of a general reaction screening approach to discover low molecular weight inhibitors of protein protein interactions. On the basis of the known pharmacophore model of SMAC mimetics, we predicted several inhibitors based on four different multicomponent reactions. The predicted inhibitors were subsequently synthesized, tested, and found to bind to the antiapoptotic protein X-linked inhibitor of apoptosis protein (XIAP) and showed cellular activity. Also the compounds are currently not highly potent. They could form a starting point for future medicinal chemistry optimization.

KW - Amino Acid Motifs

KW - Amino Acid Sequence

KW - Antineoplastic Agents

KW - Cell Line, Tumor

KW - Cell Survival

KW - Databases, Factual

KW - Drug Screening Assays, Antitumor

KW - Humans

KW - Models, Molecular

KW - Peptidomimetics

KW - Piperazines

KW - Protein Binding

KW - Stereoisomerism

KW - Structure-Activity Relationship

KW - Tetrazoles

KW - Thiazoles

KW - Thiazolidines

KW - X-Linked Inhibitor of Apoptosis Protein

U2 - 10.1021/jm101341m

DO - 10.1021/jm101341m

M3 - Article

C2 - 21241056

VL - 54

SP - 890

EP - 900

JO - Journal of Medicinal Chemistry

JF - Journal of Medicinal Chemistry

SN - 0022-2623

IS - 3

ER -

ID: 13780602